505477 | NAE Inhibitor, MLN4924 - CAS 951950-33-7 - Calbiochem

505477
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₁H₂₅N₅O₄S 951950-33-7

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      5.05477.0001
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          Glass bottle 5 mg
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          Description
          OverviewA cell-permeable AMP mimetic that targets the NEDD8-activating E1 enzyme NAE nucleotide-binding site and undergoes a NAE-catalyzed covalent NEDD8 adduct formation, the adduct in turn acts as a tight-binding, ATP-competitive NAE inhibitor (IC50 = 4.7 nM), exhibiting much reduced or little potency against UAE/UBA1, UBA6/UBE1L2, SAE, ATG7, adenosine receptors A1/A2A/A2B/A3, or a panel of 12 cellular kinases. Selectively reduces cellular Ubc12-NEDD8, but not Ubc9-SUMO or Ubc10-Ub, thioester formation (ICmax = 90 nM in HCT-116 cultures in 24 h), resulting in cullin-RING ligases substrates elevation. Shown to inhibit the growth of various cancer cells both in cultures (IC50 from 50 nM to 1.03 µM) in vitro and in murine xenograft models (30 to 60 mg/kg via s.c.) in vivo via apoptosis induction.
          Catalogue Number505477
          Brand Family Calbiochem®
          Synonyms((1S,2S,4R)-4-(4-((1S)-2,3-Dihydro-1H-inden-1-ylamino)-7H-pyrrolo[2,3-d]pyrimidin-7-yl}-2-hydroxycyclopentyl)methyl sulphamate, NEDD8-Activating Enzyme Inhibitor
          References
          ReferencesMilhollen, M.A., et al. 2010. Blood 116, 1515.
          Brownell, J.E., et al. 2010. Mol. Cell 37, 102.
          Soucy, T.A., et al. 2009. Nature 458, 73.
          Product Information
          CAS number951950-33-7
          FormLight beige solid
          Hill FormulaC₂₁H₂₅N₅O₄S
          Chemical formulaC₂₁H₂₅N₅O₄S
          ReversibleN
          Structure formula ImageStructure formula Image
          Applications
          ApplicationNAE Inhibitor, MLN4924, CAS 951950-33-7, is an AMP mimetic that forms a NAE-catalyzed NEDD8 adduct, which acts as a tight-binding, ATP-competitive NAE inhibitor (IC50 = 4.7 nM).
          Biological Information
          Primary TargetNEDD8-Activating Enzyme
          Primary Target IC<sub>50</sub>4.7 nM)
          Purity≥98% by HPLC
          Physicochemical Information
          Cell permeableY
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          Product Usage Statements
          Storage and Shipping Information
          Ship Code Ambient Temperature Only
          Toxicity Standard Handling
          Storage +2°C to +8°C
          Protect from Light Protect from light
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Milhollen, M.A., et al. 2010. Blood 116, 1515.
          Brownell, J.E., et al. 2010. Mol. Cell 37, 102.
          Soucy, T.A., et al. 2009. Nature 458, 73.
          Data Sheet

          Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

          Revision11-October-2013 JSW
          Synonyms((1S,2S,4R)-4-(4-((1S)-2,3-Dihydro-1H-inden-1-ylamino)-7H-pyrrolo[2,3-d]pyrimidin-7-yl}-2-hydroxycyclopentyl)methyl sulphamate, NEDD8-Activating Enzyme Inhibitor
          DescriptionA cell-permeable AMP mimetic that targets the NEDD8-activating E1 enzyme NAE nucleotide-binding site and undergoes a NAE-catalyzed covalent NEDD8 adduct formation, the adduct in turn acts as a tight-binding, ATP-competitive NAE inhibitor (IC50 = 4.7 nM), exhibiting much reduced or little potency against Ub-activating enzyme UAE/UBA1, Ub-like modifier activating enzyme UBA6/UBE1L2, SUMO activating enzyme SAE, Ub-like modifier activating enzyme ATG7 (IC50 = 1.5, 1.8, 8.2, and >10 µM, respectively), adenosine receptors A1/A2A/A2B/A3, or a panel of 12 cellular kinases (IC50 >10 µM). Selectively reduces cellular Ubc12-NEDD8, but not Ubc9-SUMO or Ubc10-Ub, thioester formation (ICmax = 90 nM in HCT-116 cultures in 24 h), resulting in build-up of CRLs (cullin-RING ligases) substrates CDT1, NFE2L2/NRF2, and p27, without affecting overall cellular protein turnover. Shown to inhibit the growth of cancers of various origins both in cultures (IC50 from 50 nM to 1.03 µM) in vitro and in murine xenograft models (30 to 60 mg/kg; q.d. or b.i.d via s.c.) in vivo via apoptosis induction.
          FormLight beige solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number951950-33-7
          Chemical formulaC₂₁H₂₅N₅O₄S
          Structure formulaStructure formula
          Purity≥98% by HPLC
          SolubilityDMSO (100 mg/ml). Use only fresh DMSO for reconstitution.
          Storage +2°C to +8°C
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
          Toxicity Standard Handling
          ReferencesMilhollen, M.A., et al. 2010. Blood 116, 1515.
          Brownell, J.E., et al. 2010. Mol. Cell 37, 102.
          Soucy, T.A., et al. 2009. Nature 458, 73.